JP2017528475A5 - - Google Patents
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- Publication number
- JP2017528475A5 JP2017528475A5 JP2017513759A JP2017513759A JP2017528475A5 JP 2017528475 A5 JP2017528475 A5 JP 2017528475A5 JP 2017513759 A JP2017513759 A JP 2017513759A JP 2017513759 A JP2017513759 A JP 2017513759A JP 2017528475 A5 JP2017528475 A5 JP 2017528475A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- cancer
- compound according
- pyridinyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- 125000006002 1,1-difluoroethyl group Chemical group 0.000 claims 2
- ZMLHBBXPXZXTSP-UHFFFAOYSA-N 2-fluoropropane Chemical group C[C](C)F ZMLHBBXPXZXTSP-UHFFFAOYSA-N 0.000 claims 2
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 claims 1
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 1
- 208000002699 Digestive System Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 101100381978 Mus musculus Braf gene Proteins 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
- 229940045985 antineoplastic platinum compound Drugs 0.000 claims 1
- 229960004397 cyclophosphamide Drugs 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims 1
- 229960005420 etoposide Drugs 0.000 claims 1
- 201000010231 gastrointestinal system cancer Diseases 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- HOMGKSMUEGBAAB-UHFFFAOYSA-N ifosfamide Chemical compound ClCCNP1(=O)OCCCN1CCCl HOMGKSMUEGBAAB-UHFFFAOYSA-N 0.000 claims 1
- 229960001101 ifosfamide Drugs 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003058 platinum compounds Chemical class 0.000 claims 1
- 208000000649 small cell carcinoma Diseases 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- 229960004964 temozolomide Drugs 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462049469P | 2014-09-12 | 2014-09-12 | |
| US62/049,469 | 2014-09-12 | ||
| PCT/IB2015/056986 WO2016038581A1 (en) | 2014-09-12 | 2015-09-11 | Compounds and compositions as raf kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017528475A JP2017528475A (ja) | 2017-09-28 |
| JP2017528475A5 true JP2017528475A5 (enExample) | 2018-10-18 |
| JP6678655B2 JP6678655B2 (ja) | 2020-04-08 |
Family
ID=54148595
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017513759A Active JP6678655B2 (ja) | 2014-09-12 | 2015-09-11 | Ｒａｆキナーゼ阻害剤としての化合物および組成物 |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US9573969B2 (enExample) |
| EP (1) | EP3191472B1 (enExample) |
| JP (1) | JP6678655B2 (enExample) |
| KR (1) | KR20170053686A (enExample) |
| CN (1) | CN107108671B (enExample) |
| AP (1) | AP2017009830A0 (enExample) |
| AR (1) | AR101815A1 (enExample) |
| AU (1) | AU2015313782B2 (enExample) |
| BR (1) | BR112017004741A2 (enExample) |
| CA (1) | CA2960971A1 (enExample) |
| CL (1) | CL2017000541A1 (enExample) |
| CO (1) | CO2017002292A2 (enExample) |
| CR (1) | CR20170092A (enExample) |
| CU (1) | CU20170026A7 (enExample) |
| DO (1) | DOP2017000066A (enExample) |
| EA (1) | EA031061B1 (enExample) |
| EC (1) | ECSP17021897A (enExample) |
| ES (1) | ES2729243T3 (enExample) |
| IL (1) | IL250950A0 (enExample) |
| MX (1) | MX2017003233A (enExample) |
| NI (1) | NI201700029A (enExample) |
| PE (1) | PE20171338A1 (enExample) |
| PH (1) | PH12017500416A1 (enExample) |
| SG (1) | SG11201701734QA (enExample) |
| SV (1) | SV2017005405A (enExample) |
| TN (1) | TN2017000075A1 (enExample) |
| TW (1) | TWI603977B (enExample) |
| UY (1) | UY36294A (enExample) |
| WO (1) | WO2016038581A1 (enExample) |
| ZA (1) | ZA201701633B (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014140075A1 (en) | 2013-03-14 | 2014-09-18 | Boehringer Ingelheim International Gmbh | Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| TN2016000270A1 (en) * | 2014-01-14 | 2017-10-06 | Millennium Pharm Inc | Heteroaryls and uses thereof. |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| CN108047240B (zh) | 2014-09-12 | 2020-08-04 | 勃林格殷格翰国际有限公司 | 组织蛋白酶c的螺环化合物抑制剂 |
| KR102341660B1 (ko) | 2016-09-19 | 2021-12-23 | 노파르티스 아게 | Raf 억제제 및 erk 억제제를 포함하는 치료적 조합 |
| ES2952265T3 (es) | 2017-05-02 | 2023-10-30 | Novartis Ag | Terapia combinada que comprende un inhibidor de Raf y trametinib |
| MX2020001254A (es) * | 2017-08-03 | 2020-03-20 | Novartis Ag | Combinacion terapeutica de un inhibidor tirosina quinasa del egfr de tercera generacion y un inhibidor raf. |
| CA3133812A1 (en) * | 2019-03-22 | 2020-10-01 | Kinnate Biopharma Inc. | Inhibitors of raf kinases |
| TW202106684A (zh) | 2019-05-03 | 2021-02-16 | 美商奇奈特生物製藥公司 | Raf激酶抑制劑 |
| EP3969449B1 (en) | 2019-05-13 | 2025-02-12 | Novartis AG | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer |
| CA3158530A1 (en) * | 2019-10-24 | 2021-04-29 | Stephen W. Kaldor | Inhibitors of raf kinases |
| CN114746417B (zh) * | 2019-12-06 | 2023-12-08 | 齐鲁制药有限公司 | Pan-RAF激酶抑制剂的联芳基化合物 |
| US11407737B2 (en) | 2020-09-18 | 2022-08-09 | Kinnate Biopharma Inc. | Inhibitors of RAF kinases |
| WO2022066580A1 (en) * | 2020-09-23 | 2022-03-31 | Kinnate Biopharma Inc. | Raf degrading compounds |
| WO2022081469A1 (en) | 2020-10-12 | 2022-04-21 | Kinnate Biopharma Inc. | Inhibitors of raf kinases |
| JP2024516972A (ja) * | 2021-04-23 | 2024-04-18 | キネート バイオファーマ インク． | Ｒａｆ阻害薬による癌の処置 |
| CA3216258A1 (en) * | 2021-04-23 | 2022-10-27 | Stephen W. Kaldor | Solid state forms of (s)-n-(3-(2-(((r)-1-hydroxypropan-2-yl)amino)-6-morpholinopyridin-4-yl)-4-methylphenyl)-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and salts thereof |
| CN119119062A (zh) * | 2021-05-12 | 2024-12-13 | 勃林格殷格翰国际有限公司 | 作为cGAS抑制剂的具有N-连接环状取代基的吡啶衍生物 |
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